Z-Guggulsterone
(Synonyms: 孕二烯二酮) 目录号 : GC10195
Z-Guggulsterone 是阿育吠陀药用植物 Commiphora mukul 的一种成分，在体外和体内抑制血管生成，IC50 值为 1740、1000、220 和 >； 50000 nM 用于糖皮质激素、盐皮质激素、雄激素和法尼醇 X 受体 。
Cas No.:39025-23-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Z-Guggulsterone, a component of the Ayurvedic medicinal plant Commiphora mukul, suppresses angiogenesis in vitro and in vivo with IC50 values of 1740, 1000, 220 and > 50000 nM for glucocorticoid, mineralocorticoid, androgen and farnesoid X receptors [1].
Bcl-2 protein expression was significantly decreased, and active caspase-3 and Bax protein expression was increased in SGC-7901 cells incubated with z-guggulsterone. The content of TNF-α was significantly increased, and the contents of VEGF and TGF-β1 were decreased in SGC-7901 cells incubated with z-guggulsterone[3]. In human umbilical vein endothelial cells (HUVEC) and DU145 cells, z-guggulsterone (5, 10 and 20 μM) significantly decrease cell migration in a concentration- and time-dependent manner, inhibiting capillary-like tube formation[4]. Z-guggulsterone (30 μM) simultaneously inhibited the expression of PXR and MDR1 at 24 h in human brain-derived microvessel endothelial cells (hBDMECs)[5].Z-guggulsterone attenuated TREM-1-mediated macrophage hyperactivation by suppressing TREM-1 expression and NF-κB and AP-1 activation[2].
Programmed death-ligand 1 (PD-L1) is an immune checkpoint molecule, that is overexpressed in non-small cell lung cancer (NSCLC) and has been associated with the response to anti-PD-1/PD-L1 immunotherapy.In vivo, Z-Guggulsterone treatment dose-dependently increased PD-L1 expression levels in mouse LLC tumor models[6]. Z-Guggulsterone significantly alleviated neurological deficits, infarct volume and histopathological damage in MCAO rats. Z-Guggulsterone successfully inhibited oxidative stress and inflammatory response in oxygen-glucose deprivation (OGD) treated neurons. Z-Guggulsterone exerted neuroprotective property through alleviated oxidative stress and inflammation via inhibiting the TXNIP/NLRP3 axis[7].
References:
[1]: Burris TP, Montrose C, et,al. The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Mol Pharmacol. 2005 Mar;67(3):948-54. doi: 10.1124/mol.104.007054. Epub 2004 Dec 15. PMID: 15602004.
[2]: Che X, Park KC, et,al.Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139. doi: 10.1152/ajpgi.00027.2018. Epub 2018 Mar 15. PMID: 29543509.
[3]: Lv R, Zhu M, et,al. Z-Guggulsterone Induces Apoptosis in Gastric Cancer Cells through the Intrinsic Mitochondria-Dependent Pathway. ScientificWorldJournal. 2021 Jan 4;2021:3152304. doi: 10.1155/2021/3152304. PMID: 33488300; PMCID: PMC7801056.
[4]: Xiao D, Singh SV. z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Mol Cancer Ther. 2008 Jan;7(1):171-80. doi: 10.1158/1535-7163.MCT-07-0491. PMID: 18202020.
[5]: Xu HB, Tang ZQ, et,al. Z-guggulsterone regulates MDR1 expression mainly through the pregnane X receptor-dependent manner in human brain microvessel endothelial cells. Eur J Pharmacol. 2020 May 5;874:173023. doi: 10.1016/j.ejphar.2020.173023. Epub 2020 Feb 19. PMID: 32087256.
[6]: Tian H, Gui Y, et,al. Z-guggulsterone induces PD-L1 upregulation partly mediated by FXR, Akt and Erk1/2 signaling pathways in non-small cell lung cancer. Int Immunopharmacol. 2021 Apr;93:107395. doi: 10.1016/j.intimp.2021.107395. Epub 2021 Jan 30. PMID: 33529916.
[7]: Liu T, Wang W, et,al. Z-Guggulsterone alleviated oxidative stress and inflammation through inhibiting the TXNIP/NLRP3 axis in ischemic stroke. Int Immunopharmacol. 2020 Dec;89(Pt B):107094. doi: 10.1016/j.intimp.2020.107094. Epub 2020 Oct 28. PMID: 33129097.
Z-Guggulsterone 是阿育吠陀药用植物 Commiphora mukul 的一种成分，在体外和体内抑制血管生成，IC50 值为 1740、1000、220 和 >； 50000 nM 用于糖皮质激素、盐皮质激素、雄激素和法尼醇 X 受体 [1]。
在与 z-guggulsterone 孵育的 SGC-7901 细胞中，Bcl-2 蛋白表达显着降低，活性 caspase-3 和 Bax 蛋白表达增加。 z-guggulsterone[3]培养的SGC-7901细胞TNF-α含量显着升高，VEGF和TGF-β1含量显着降低。在人脐静脉内皮细胞 (HUVEC) 和 DU145 细胞中，z-guggulsterone（5、10 和 20 μM）以浓度和时间依赖性方式显着降低细胞迁移，抑制毛细管样管形成[4] 。 Z-guggulsterone (30 μM) 在 24 小时时同时抑制人脑微血管内皮细胞 (hBDMEC) 中 PXR 和 MDR1 的表达[5]。Z-guggulsterone 减弱 TREM-1 介导的巨噬细胞通过抑制 TREM-1 表达和 NF-κB 和 AP-1 激活来过度激活[2]。
程序性死亡配体 1 (PD-L1) 是一种免疫检查点分子，在非小细胞肺癌 (NSCLC) 中过度表达，并且与抗 PD-1/PD-L1 免疫疗法的反应有关.在体内，Z-Guggulsterone 剂量依赖性地增加了小鼠 LLC 肿瘤模型中的 PD-L1 表达水平[6]。 Z-Guggulsterone 显着减轻 MCAO 大鼠的神经功能缺损、梗塞体积和组织病理学损伤。 Z-Guggulsterone 成功抑制氧-葡萄糖剥夺 (OGD) 处理的神经元中的氧化应激和炎症反应。 Z-Guggulsterone 通过抑制 TXNIP/NLRP3 轴来减轻氧化应激和炎症，发挥神经保护作用[7]。
| Cell experiment [1]: | |
|
Cell lines |
Bone marrow-derived macrophage (BMDM) |
|
Preparation Method |
Cells were incubated with Z-Guggulsterone at increasing concentrations (0, 0.5, 5, and 20 M) for 1 h and then simulated with LPS in the presence or absence of TREM-1 agonist antibody for the indicated time. |
|
Reaction Conditions |
0.5-20uM Z-Guggulsterone for 1h |
|
Applications |
Z-Guggulsterone attenuates TREM-1-mediated hyperactivation of macrophages through inhibition of TREM-1 expression and NF-κB and AP-1 activation. |
| Animal experiment [2]: | |
|
Animal models |
IL-10, TLR4, and MyD88 deficient mice |
|
Preparation Method |
Z-Guggulsterone were administered orally at 100 mg/kg once daily after TNBS administration for 4 days or throughout the experiment. The mice were monitored for weight loss, fecal consistency, presence of crude blood in the feces or anus, and overall mortality |
|
Dosage form |
100 mg/kg Z-Guggulsterone orally administered once daily for 4 days |
|
Applications |
Z-Guggulsterone improves colitis in mice by regulating macrophage phenotype through IL-10 and TLR4/MyD88 pathways. |
|
References: [1]: Che X, Park KC, et,al. Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139. doi: 10.1152/ajpgi.00027.2018. Epub 2018 Mar 15. PMID: 29543509. | |
| Cas No. | 39025-23-5 | SDF | |
| 别名 | 孕二烯二酮 | ||
| 化学名 | (8S,9R,10R,13R,14S,Z)-17-ethylidene-10,13-dimethyl-7,8,9,10,11,12,13,14,15,17-decahydro-1H-cyclopenta[a]phenanthrene-3,16(2H,6H)-dione | ||
| Canonical SMILES | O=C1C[C@H]([C@@](/C1=C/C)(C)CC2)[C@@H](CC3)[C@@H]2[C@](CC4)(C)C3=CC4=O | ||
| 分子式 | C21H28O2 | 分子量 | 312.45 |
| 溶解度 | ≥ 3.12mg/mL in DMSO with ultrasonic and warming | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2005 mL | 16.0026 mL | 32.0051 mL |
| 5 mM | 0.6401 mL | 3.2005 mL | 6.401 mL |
| 10 mM | 0.3201 mL | 1.6003 mL | 3.2005 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet